Arenimycin, an antibiotic effective against rifampin- and methicillin-resistant Staphylococcus aureus from the marine actinomycete Salinispora arenicola.
Arenimycin, an antibiotic effective against rifampin- and methicillin-resistant Staphylococcus aureus from the marine actinomycete Salinispora arenicola.
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DOI：
10.1038/ja.2009.114
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发表时间：
2010-01
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耐药细菌感染的发生率继续增加，仍然是对人类健康的严重威胁。2007年，美国疾病控制及预防中心（Centers for Disease Control and Prevention，CDC）报告，单是耐甲氧西林金黄色葡萄球菌（MRSA）所引致的严重感染个案，每年便接近10万宗，而相关的死亡个案亦接近19 000宗，比同年美国因艾滋病病毒/艾滋病（Human Immunodeficiency Virus/Acquired Immunodeficiency Syndrome，HIV/AIDS）而引致的死亡人数还要多。1海洋天然产物提供了丰富的生物活性分子来源，这些生物活性分子在开发新的药物制剂方面具有潜在价值。2特别是海洋细菌已被证明是小分子的良好来源，绝大多数化合物是从属于放线菌目（放线菌）的化学多产革兰氏阳性细菌中发现的。在已报道的新型天然产物的海洋放线菌中，专性海洋属Salinispora产生了一系列令人印象深刻的结构多样的化合物，包括Salinosporamide A，其目前正用于治疗癌症的临床试验。3这些化合物以物种特异性模式产生，包括利福霉素类的强效抗生素，这些抗生素在沙生盐孢菌提取物中一直被观察到。4为了从大量的S.在一种耐利福平的MRSA菌株中，我们使用来自于除利福霉素之外的化合物的提取物来筛选抗生素活性。来自大量富集了从盐孢属物种收集的提取物的文库的2400个粗提取物。只有六个（0.3%）的提取物显示出有前途的生物活性对利福平耐药MRSA。在这些活性提取物中，S.沙生菌株
The incidence of infections by drug-resistant bacteria continues to increase and remains a serious threat to human health. In 2007, the US CDC (Centers for Disease Control and Prevention) reported that the number of serious infections caused by methicillin-resistant Staphylococcus aureus (MRSA) alone was close to 100000 a year, with almost 19 000 related fatalities, a number that is larger than the US death toll attributed to HIV/AIDS (human immunodeficiency virus/acquired immunodeficiency syndrome) in the same year. 1 Marine natural products offer a rich source of poorly explored bioactive molecules that are of potential value in the development of new pharmaceutical agents. 2 Marine bacteria in particular have proven to be a good source of small molecules, with the vast majority of compounds being discovered from chemically prolific Gram+ bacteria belonging to the order Actinomycetales (actinomycetes). Of the marine actinomycetes from which novel natural products have been reported, the obligate marine genus Salinispora has yielded an impressive array of structurally diverse compounds including salinosporamide A, which is currently being used in clinical trials for the treatment of cancer. 3 These compounds are produced in species-specific patterns and include potent antibiotics in the rifamycin class, which are consistently observed in extracts of Salinispora arenicola. 4 In an effort to discover new antibiotics from a large collection of S. arenicola strains, a rifampin-resistant strain of MRSA was used to screen extracts for antibiotic activities that are derived from compounds other than rifamycins.In total, we screened ca. 2400 crude extracts from a library that was heavily enriched with extracts collected from Salinispora species. Only six (0.3%) of the extracts showed promising biological activity against rifampin-resistant MRSA. Among these active extracts, a liquid chromatography (LC) MS analysis of the extract of S. arenicola strain
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影响因子：
1.1
作者：
GERBER, NN;LECHEVALIER, MP
通讯作者：
LECHEVALIER, MP
影响因子：
3.3
作者：
Martin, R;Sterner, O;Minas, W
通讯作者：
Minas, W
影响因子：
3.3
作者：
YASUZAWA, T;YOSHIDA, M;SANO, H
通讯作者：
SANO, H
影响因子：
4.4
作者：
Jensen, Paul R.;Williams, Philip G.;Fenical, William
通讯作者：
Fenical, William
影响因子：
5.1
作者：
Snipes, Carl E.;Duebelbeis, Dennis O.;Graupner, Paul R.
通讯作者：
Graupner, Paul R.